| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary target is central inhibitory alpha-adrenergic receptors. Methyldopa is metabolized to alpha-methylnorepinephrine, which stimulates central inhibitory alpha-adrenergic receptors, leading to reduced sympathetic outflow and decreased arterial pressure. It also acts as a false neurotransmitter, replacing norepinephrine in synaptic vesicles. It inhibits aromatic-amino-acid decarboxylase.
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|---|---|
| ln Vitro |
L-α-Methyldopa inhibits dopa decarboxylase and depletes animal tissues of norepinephrine. It causes a net reduction in tissue concentrations of serotonin, dopamine, norepinephrine, and epinephrine. The antihypertensive activity appears to be due solely to the L-isomer. About twice the dose of the racemate is required for equal antihypertensive effect. It has no direct effect on cardiac function.
|
| ln Vivo |
Methyldopa hydrochloride (L-(-)-α-methyldopa hydrochloride; 200 mg/kg; intraperitoneally) lessens hyperglycemic responses in the first two hours following dieldrin administration [2].
In vivo, methyldopa reduces both supine and standing blood pressure. The maximum decrease in blood pressure occurs 4-6 hours after oral dosage. Once an effective dosage level is attained, a smooth blood pressure response occurs in 12-24 hours. After withdrawal, blood pressure returns to pretreatment levels within 24-48 hours. It usually does not reduce glomerular filtration rate or renal blood flow. |
| Enzyme Assay |
Aromatic-amino-acid decarboxylase activity assays use tissue homogenates or purified enzyme. The enzyme is incubated with L-α-methyldopa and a radiolabeled substrate (e.g., L-DOPA). Decarboxylation is measured by detecting the release of 14CO2 or by HPLC quantification of the product. IC50 values are calculated from dose-response curves.
|
| Cell Assay |
Cell-based assays for methyldopa activity use PC12 cells or primary neurons. Cells are treated with L-α-methyldopa (0.1-100 µM) for 24-48 h. Catecholamine levels (norepinephrine, dopamine) in cells and medium are measured by HPLC with electrochemical detection. Cell viability is assessed by MTT assay.
|
| Animal Protocol |
Animal/Disease Models: 60-day-old male rats [2]
Doses: 200 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Within 30 minutes after administration, the plasma glucose concentration of rats exposed to dieldrin diminished by 24% . In vivo, methyldopa is tested in hypertensive animal models (spontaneously hypertensive rats, renal hypertensive rats). The compound is administered orally (10-100 mg/kg) daily for 2-8 weeks. Blood pressure is measured by tail cuff or telemetry. Tissue catecholamine levels are measured by HPLC. Cardiac and renal function are assessed histologically. |
| References |
|
| Molecular Formula |
C10H13NO4.HCL
|
|---|---|
| Molecular Weight |
247.67546
|
| Exact Mass |
247.061
|
| CAS # |
884-39-9
|
| Related CAS # |
Methyldopa hydrate;41372-08-1;Methyldopa;555-30-6;Methyldopa-d3 hydrochloride
|
| PubChem CID |
3083659
|
| Appearance |
Typically exists as solid at room temperature
|
| Source |
Endogenously produced metabolite
|
| LogP |
1.944
|
| tPSA |
103.78
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
16
|
| Complexity |
246
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
OC1=C(O)C=CC(C[C@@](C)(C(O)=O)N)=C1.Cl
|
| InChi Key |
NLRUDGHSXOEXCE-PPHPATTJSA-N
|
| InChi Code |
InChI=1S/C10H13NO4.ClH/c1-10(11,9(14)15)5-6-2-3-7(12)8(13)4-6;/h2-4,12-13H,5,11H2,1H3,(H,14,15);1H/t10-;/m0./s1
|
| Chemical Name |
(2S)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0375 mL | 20.1873 mL | 40.3747 mL | |
| 5 mM | 0.8075 mL | 4.0375 mL | 8.0749 mL | |
| 10 mM | 0.4037 mL | 2.0187 mL | 4.0375 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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